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Targeting epigenetic networks with polypharmacology: a new avenue to tackle cancer

Gianluigi Franci1, Marco Miceli, Lucia Altucci

  • 1Seconda Università di Napoli, Napoli, Italy.

Epigenomics
|November 30, 2011
PubMed

Insights

Epigenetic modifications regulate gene expression without altering DNA. Targeting these epigenetic enzymes offers new cancer treatment strategies, potentially through poly-pharmacology.

Area of Science:

  • Molecular Biology
  • Genetics
  • Biochemistry

Background:

  • Epigenetics involves gene expression modulation beyond DNA sequence.
  • Epigenetic control relies on enzymes modifying chromatin structure.
  • Dysregulation of these enzymes is linked to diseases like cancer.

Purpose of the Study:

  • To explore epigenetic enzymes as therapeutic targets in cancer.
  • To evaluate the potential of poly-pharmacological approaches in epigenetic cancer therapy.

Main Methods:

  • Review of epigenetic mechanisms and enzyme functions.
  • Analysis of existing and potential small-molecule inhibitors targeting epigenetic enzymes.
  • Discussion of poly-pharmacological strategies versus single-target approaches.

Main Results:

  • DNA methyltransferase and histone deacetylase inhibitors are approved cancer treatments.
  • Other epigenetic enzymes (e.g., MS-275, SAHA) show disease associations and are targeted.
  • Poly-pharmacological targeting of multiple epigenetic enzymes is proposed as a 'smart' cancer treatment.

Conclusions:

  • Epigenetic enzyme inhibitors represent a novel therapeutic avenue for cancer.
  • Targeting multiple epigenetic enzymes simultaneously may offer advantages over single-target therapies.

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